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Showing drug card for Clopidogrel (DB00758)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-06-23 18:08:02
Primary Accession Number DB00758
Secondary Accession Number
  • APRD00444
Name Clopidogrel
Drug Type
  • Approved
  • Small Molecule
Description Clopidogrel, an antiplatelet agent structurally and pharmacologically similar to ticlopidine, is used to reduce atherosclerotic events such as myocardial infarction, stroke, and vascular death in patients who have had a recent stroke, recent MI, or have established peripheral vascular disease.
Synonyms Not Available
Brand Names
  1. Clopidogrel [Ban:Inn]
  2. Clopidogrel sulfate
  3. Plavix
Brand Mixtures Not Available
Chemical IUPAC Name methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate
Chemical Formula C16H16ClNO2S
Chemical Structure Structure
CAS Registry Number 113665-84-2
InChI Identifier InChI=1/C16H16ClNO2S/c1-20-16(19)15(12-4-2-3-5-13(12)17)18-8-6-14-11(10-18)7-9-21-14/h2-5,7,9,15H,6,8,10H2,1H3/t15-/m0/s1
InChI Key GKTWGGQPFAXNFI-HNNXBMFYBE
KEGG Drug D00769 Link Image
KEGG Compound Not Available
PubChem Compound 60606 Link Image
PubChem Substance 196885 Link Image
ChEBI ID Not Available
PharmGKB ID PA449053 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02238682 Link Image
RxList Link http://www.rxlist.com/cgi/generic/clopidog.htm Link Image
PDRhealth Link http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/pla1338.shtml Link Image
Wikipedia Link http://en.wikipedia.org/wiki/Clopidogrel Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference D. Aubert et al.; U.S. Pat. 4,529,596(1985)
Average Molecular Weight 321.8220
Monoisotopic Molecular Weight 321.0590
State Solid
Melting Point 158oC
Experimental Water Solubility 50.78 mg/L Source: PhysProp
Predicted Water Solubility 1.18e-02 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 2.5 Source: PhysProp
Predicted LogP 3.84 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.43 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID Not Available
Isomeric SMILES COC(=O)[C@@H](N1CCC2=C(C1)C=CS2)C1=CC=CC=C1Cl
Canonical SMILES COC(=O)C(N1CCC2=C(C1)C=CS2)C1=CC=CC=C1Cl
Drug Category
  • Antiplatelet Agents
  • Fibrinolytic Agents
  • Platelet Aggregation Inhibitors
ATC Codes
AHFS Codes
  • 20:12.18
Indication For the reduction of atherosclerotic events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease
Pharmacology Clopidogrel, an antiplatelet agent structurally and pharmacologically similar to ticlopidine, is used to reduce atherosclerotic events such as myocardial infarction, stroke, and vascular death in patients who have had a recent stroke, recent MI, or have established peripheral vascular disease.
Mechanism of Action The active metabolite of clopidogrel prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. It is proposed that the inhibition involves a defect in the mobilization from the storage sites of the platelet granules to the outer membrane. No direct interference occurs with the GPIIb/IIIa receptor. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation. By blocking the amplification of platelet activation by released ADP, platelet aggregation induced by agonists other than ADP is also inhibited by the active metabolite of clopidogrel.
Absorption Absorption is at least 50% based on urinary excretion of clopidogrel-related metabolites. Bioavailability has not been found to be affected by food.
Toxicity Symptoms of acute toxicity include vomiting (in baboons), prostration, difficult breathing, and gastrointestinal hemorrhage.
Protein Binding 98%
Biotransformation Hepatic, extensive and rapid, by hydrolysis to the main circulating metabolite, a carboxylic acid derivative, which accounts for approximately 85% of the circulating drug-related compounds. A glucuronic acid derivative of the carboxylic acid derivative has also been found in plasma and urine. Neither the parent compound nor the carboxylic acid derivative has a platelet inhibiting effect.
Half Life Carboxylic acid derivative: 8 hours (after single and multiple doses). Covalent binding to platelets has accounted for 2% of radiolabeled clopidogrel with a half-life of 11 days.
Dosage Forms
Form Route
Tablet Oral
Patient Information Show Link Image
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions Not Available
Food Interactions
  • Take without regard to meals.
Pathways
Name SMPDB Link KEGG Link
Clopidogrel Pathway SMP00260 Link Image
General References
  1. Chan FK, Ching JY, Hung LC, Wong VW, Leung VK, Kung NN, Hui AJ, Wu JC, Leung WK, Lee VW, Lee KK, Lee YT, Lau JY, To KF, Chan HL, Chung SC, Sung JJ: Clopidogrel versus aspirin and esomeprazole to prevent recurrent ulcer bleeding. N Engl J Med. 2005 Jan 20;352(3):238-44. [PubMed Link Image]
  2. Drugs.com Link Image
  3. Wikipedia Link Image
  4. RxList Link Image
  5. PDRhealth Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 3A5 (CYP3A5)
  2. Cytochrome P450 3A4 (CYP3A4)
  3. Cytochrome P450 2B6 (CYP2B6)
Targets
  1. P2Y purinoceptor 12
  2. Cytochrome P450 3A3
  3. P-selectin
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 3A5 (CYP3A5)
Enzyme 1 Gene Name CYP3A5
Enzyme 1 SwissProt ID P20815 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P20815|CP3A5_HUMAN Cytochrome P450 3A5 
MDLIPNLAVETWLLLAVSLVLLYLYGTRTHGLFKRLGIPGPTPLPLLGNVLSYRQGLWKF
DTECYKKYGKMWGTYEGQLPVLAITDPDVIRTVLVKECYSVFTNRRSLGPVGFMKSAISL
AEDEEWKRIRSLLSPTFTSGKLKEMFPIIAQYGDVLVRNLRREAEKGKPVTLKDIFGAYS
MDVITGTSFGVNIDSLNNPQDPFVESTKKFLKFGFLDPLFLSIILFPFLTPVFEALNVSL
FPKDTINFLSKSVNRMKKSRLNDKQKHRLDFLQLMIDSQNSKETESHKALSDLELAAQSI
IFIFAGYETTSSVLSFTLYELATHPDVQQKLQKEIDAVLPNKAPPTYDAVVQMEYLDMVV
NETLRLFPVAIRLERTCKKDVEINGVFIPKGSMVVIPTYALHHDPKYWTEPEEFRPERFS
KKKDSIDPYIYTPFGTGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLDTQG
LLQPEKPIVLKVDSRDGTLSGE
Phase 1 Metabolizing Enzyme 2 [top]
Enzyme 2 Name Cytochrome P450 3A4 (CYP3A4)
Enzyme 2 Gene Name CYP3A4
Enzyme 2 SwissProt ID P08684 Link Image
Enzyme 2 SNPs SNPJam Report Link Image
Enzyme 2 Protein Sequence >sp|P08684|CP3A4_HUMAN Cytochrome P450 3A4 (EC 1.14.13.67) 
ALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMFD
MECHKKYGKVWGFYDGQQPVLAITDPDMIKTVLVKECYSVFTNRRPFGPVGFMKSAISIA
EDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRREAETGKPVTLKDVFGAYSM
DVITSTSFGVNIDSLNNPQDPFVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICVF
PREVTNFLRKSVKRMKESRLEDTQKHRVDFLQLMIDSQNSKETESHKALSDLELVAQSII
FIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMVVN
ETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERFSK
KNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSLGG
LLQPEKPVVLKVESRDGTVSGA
Phase 1 Metabolizing Enzyme 3 [top]
Enzyme 3 Name Cytochrome P450 2B6 (CYP2B6)
Enzyme 3 Gene Name CYP2B6
Enzyme 3 SwissProt ID P20813 Link Image
Enzyme 3 SNPs SNPJam Report Link Image
Enzyme 3 Protein Sequence >sp|P20813|CP2B6_HUMAN Cytochrome P450 2B6 (EC 1.14.14.1) 
MELSVLLFLALLTGLLLLLVQRHPNTHDRLPPGPRPLPLLGNLLQMDRRGLLKSFLRFRE
KYGDVFTVHLGPRPVVMLCGVEAIREALVDKAEAFSGRGKIAMVDPFFRGYGVIFANGNR
WKVLRRFSVTTMRDFGMGKRSVEERIQEEAQCLIEELRKSKGALMDPTFLFQSITANIIC
SIVFGKRFHYQDQEFLKMLNLFYQTFSLISSVFGQLFELFSGFLKYFPGAHRQVYKNLQE
INAYIGHSVEKHRETLDPSAPKDLIDTYLLHMEKEKSNAHSEFSHQNLNLNTLSLFFAGT
ETTSTTLRYGFLLMLKYPHVAERVYREIEQVIGPHRPPELHDRAKMPYTEAVIYEIQRFS
DLLPMGVPHIVTQHTSFRGYIIPKDTEVFLILSTALHDPHYFEKPDAFNPDHFLDANGAL
KKTEAFIPFSLGKRICLGEGIARAELFLFFTTILQNFSMASPVAPEDIDLTPQECGVGKI
PPTYQIRFLPR
Drug Target 1 [top]
Target 1 ID 122
Target 1 Name P2Y purinoceptor 12
Target 1 Synonyms
  1. ADP-glucose receptor
  2. ADPG-R
  3. P2T(AC)
  4. P2Y(AC)
  5. P2Y(ADP)
  6. P2Y(cyc)
  7. P2Y12
  8. P2Y12 platelet ADP receptor
  9. SP1999
Target 1 Gene Name P2RY12
Target 1 Protein Sequence >P2Y purinoceptor 12 
MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI
IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI
DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS
EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI
IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF
LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
Target 1 Number of Residues 347
Target 1 Molecular Weight 39439
Target 1 Theoretical pI 9.99
Target 1 GO Classification
Function
nucleotide receptor activity, G-protein coupled
purinergic nucleotide receptor activity, G-protein coupled
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
rhodopsin-like receptor activity
Process
cellular process
cell communication
signal transduction
cell surface receptor linked signal transduction
G-protein coupled receptor protein signaling pathway
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 1 General Function Involved in rhodopsin-like receptor activity
Target 1 Specific Function Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Involved in platelets aggregation
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • 26-46
  • 59-79
  • 100-120
  • 143-163
  • 192-212
  • 234-254
  • 282-302
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 12083902 Link Image
Target 1 UniProtKB/Swiss-Prot ID Q9H244 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name P2Y12_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 1 Gene Sequence >1029 bp 
ATGCAAGCCGTCGACAACCTCACCTCTGCGCCTGGGAACACCAGTCTGTGCACCAGAGAC
TACAAAATCACCCAGGTCCTCTTCCCACTGCTCTACACTGTCCTGTTTTTTGTTGGACTT
ATCACAAATGGCCTGGCGATGAGGATTTTCTTTCAAATCCGGAGTAAATCAAACTTTATT
ATTTTTCTTAAGAACACAGTCATTTCTGATCTTCTCATGATTCTGACTTTTCCATTCAAA
ATTCTTAGTGATGCCAAACTGGGAACAGGACCACTGAGAACTTTTGTGTGTCAAGTTACC
TCCGTCATATTTTATTTCACAATGTATATCAGTATTTCATTCCTGGGACTGATAACTATC
GATCGCTACCAGAAGACCACCAGGCCATTTAAAACATCCAACCCCAAAAATCTCTTGGGG
GCTAAGATTCTCTCTGTTGTCATCTGGGCATTCATGTTCTTACTCTCTTTGCCTAACATG
ATTCTGACCAACAGGCAGCCGAGAGACAAGAATGTGAAGAAATGCTCTTTCCTTAAATCA
GAGTTCGGTCTAGTCTGGCATGAAATAGTAAATTACATCTGTCAAGTCATTTTCTGGATT
AATTTCTTAATTGTTATTGTATGTTATACACTCATTACAAAAGAACTGTACCGGTCATAC
GTAAGAACGAGGGGTGTAGGTAAAGTCCCCAGGAAAAAGGTGAACGTCAAAGTTTTCATT
ATCATTGCTGTATTCTTTATTTGTTTTGTTCCTTTCCATTTTGCCCGAATTCCTTACACC
CTGAGCCAAACCCGGGATGTCTTTGACTGCACTGCTGAAAATACTCTGTTCTATGTGAAA
GAGAGCACTCTGTGGTTAACTTCCTTAAATGCATGCCTGGATCCGTTCATCTATTTTTTC
CTTTGCAAGTCCTTCAGAAATTCCTTGATAAGTATGCTGAAGTGCCCCAATTCTGCAACA
TCTCTGTCCCAGGACAATAGGAAAAAAGAACAGGATGGTGGTGACCCAAATGAAGAGACT
CCAATGTAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID P2RY12 Link Image
Target 1 GenAtlas ID P2RY12 Link Image
Target 1 HGNC ID HGNC:18124 Link Image
Target 1 Chromosome Location 3
Target 1 Locus 3q24-q25
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Zhang FL, Luo L, Gustafson E, Lachowicz J, Smith M, Qiao X, Liu YH, Chen G, Pramanik B, Laz TM, Palmer K, Bayne M, Monsma FJ Jr: ADP is the cognate ligand for the orphan G protein-coupled receptor SP1999. J Biol Chem. 2001 Mar 16;276(11):8608-15. Epub 2000 Dec 4. [PubMed Link Image]
  2. Hollopeter G, Jantzen HM, Vincent D, Li G, England L, Ramakrishnan V, Yang RB, Nurden P, Nurden A, Julius D, Conley PB: Identification of the platelet ADP receptor targeted by antithrombotic drugs. Nature. 2001 Jan 11;409(6817):202-7. [PubMed Link Image]
  3. Takasaki J, Kamohara M, Saito T, Matsumoto M, Matsumoto S, Ohishi T, Soga T, Matsushime H, Furuichi K: Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor. Mol Pharmacol. 2001 Sep;60(3):432-9. [PubMed Link Image]
  4. Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S: Identification of G protein-coupled receptor genes from the human genome sequence. FEBS Lett. 2002 Jun 5;520(1-3):97-101. [PubMed Link Image]
Target 1 Drug References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed Link Image]
  2. Dorsam RT, Murugappan S, Ding Z, Kunapuli SP: Clopidogrel: Interactions with the P2Y12 Receptor and Clinical Relevance. Hematology. 2003 Dec;8(6):359-65. [PubMed Link Image]
  3. Herbert JM, Savi P: P2Y12, a new platelet ADP receptor, target of clopidogrel. Semin Vasc Med. 2003 May;3(2):113-22. [PubMed Link Image]
  4. Taubert D, Kastrati A, Harlfinger S, Gorchakova O, Lazar A, von Beckerath N, Schomig A, Schomig E: Pharmacokinetics of clopidogrel after administration of a high loading dose. Thromb Haemost. 2004 Aug;92(2):311-6. [PubMed Link Image]
  5. Wang L, Jacobsen SE, Bengtsson A, Erlinge D: P2 receptor mRNA expression profiles in human lymphocytes, monocytes and CD34+ stem and progenitor cells. BMC Immunol. 2004 Aug 3;5:16. [PubMed Link Image]
  6. Wihlborg AK, Wang L, Braun OO, Eyjolfsson A, Gustafsson R, Gudbjartsson T, Erlinge D: ADP receptor P2Y12 is expressed in vascular smooth muscle cells and stimulates contraction in human blood vessels. Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1810-5. Epub 2004 Aug 12. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 1337
Target 2 Name Cytochrome P450 3A3
Target 2 Synonyms
  1. CYPIIIA3
  2. EC 1.14.14.1
  3. HLp
Target 2 Gene Name CYP3A3
Target 2 Protein Sequence >Cytochrome P450 3A3 
MALIPDLAMETWLLLAVSLVLLYLYGTHSHGLFKKLGIPGPTPLPFLGNILSYHKGFCMF
DMECHKKYGKVWGFYDGQQPVLAITDPDMIKLVLVKECYSVFTNREPFGPVGFMKSAISI
AEDEEWKRLRSLLSPTFTSGKLKEMVPIIAQYGDVLVRNLRRERETGKPVTLKDVFGAYS
MDVITSSSFGVNVDSLNNPQDPLVENTKKLLRFDFLDPFFLSITVFPFLIPILEVLNICV
FPREVTNFLRKAVKRMKESRLEDTQKHRVDFLQLMIDSHKNSKETESHKALSDLELVAQS
IIFIFAGYETTSSVLSFIMYELATHPDVQQKLQEEIDAVLPNKAPPTYDTVLQMEYLDMV
VNETLRLFPIAMRLERVCKKDVEINGMFIPKGWVVMIPSYALHRDPKYWTEPEKFLPERF
SKKNKDNIDPYIYTPFGSGPRNCIGMRFALMNMKLALIRVLQNFSFKPCKETQIPLKLSL
GGLLQPEKPVVLKVESRDGTVSGA
Target 2 Number of Residues 512
Target 2 Molecular Weight 57560
Target 2 Theoretical pI 8.25
Target 2 GO Classification
Function
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
tetrapyrrole binding
heme binding
binding
ion binding
cation binding
transition metal ion binding
iron ion binding
catalytic activity
oxidoreductase activity
monooxygenase activity
Process
physiological process
metabolism
cellular metabolism
generation of precursor metabolites and energy
electron transport
Component
Not Available
Target 2 General Function Secondary metabolites biosynthesis, transport and catabolism
Target 2 Specific Function Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics
Target 2 Pathways
Name SMPDB Link KEGG Link
Fatty acid metabolism SMP00051 Link Image map00071 Link Image
Target 2 Reactions
  • RH + reduced flavoprotein + O2 = ROH + oxidized flavoprotein + H2O
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 219963 Link Image
Target 2 UniProtKB/Swiss-Prot ID P05184 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name CP3A3_HUMAN Link Image
Target 2 PDB ID 1TQN Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Endoplasmic reticulum
  • endoplasmic reticulum membrane
  • peripheral membrane protein
Target 2 Gene Sequence >1515 bp 
ATGGCTCTCATCCCAGACTTGGCCATGGAAACCTGGCTTCTCCTGGCTGTCAGCCTGGTG
CTCCTCTATCTATATGGAACCCATTCACATGGACTTTTTAAGAAGCTTGGAATTCCAGGG
CCCACACCTCTGCCTTTTTTGGGAAATATTTTGTCCTACCATAAGGGCTTTTGTATGTTT
GACATGGAATGTCATAAAAAGTATGGAAAAGTGTGGGGCTTTTATGATGGTCAACAGCCT
GTGCTGGCTATCACAGATCCTGACATGATCAAACTAGTGCTAGTGAAAGAATGTTATTCT
GTCTTCACAAACCGCGAGCCTTTTGGTCCAGTGGGATTTATGAAAAGTGCCATCTCTATA
GCTGAGGATGAAGAATGGAAGAGATTACGATCATTGCTGTCTCCAACCTTCACCAGTGGA
AAACTCAAGGAGATGGTCCCTATCATTGCCCAGTATGGAGATGTGTTGGTGAGAAATCTG
AGGCGGGAACGAGAGACAGGCAAGCCTGTCACCTTGAAAGACGTCTTTGGGGCCTACAGC
ATGGATGTGATCACTAGCTCATCATTTGGAGTGAACGTCGACTCTCTCAACAATCCACAG
GACCCCCTTGTGGAAAACACCAAGAAGCTTTTAAGATTTGATTTTTTGGATCCATTCTTT
CTCTCAATAACAGTCTTTCCATTCCTCATCCCAATTCTTGAAGTATTAAATATCTGTGTG
TTTCCAAGAGAAGTTACAAATTTTTTAAGAAAAGCTGTAAAAAGGATGAAAGAAAGTCGC
CTCGAAGATACACAAAAGCACCGAGTGGATTTCCTTCAGCTGATGATTGACTCTCATAAG
AATTCAAAAGAAACTGAGTCCCACAAAGCTCTGTCCGATCTGGAGCTCGTGGCCCAATCA
ATTATCTTTATTTTTGCTGGCTATGAAACCACGAGCAGTGTTCTCTCCTTCATTATGTAT
GAACTGGCCACTCACCCTGATGTCCAGCAGAAACTGCAGGAGGAAATTGATGCAGTTTTA
CCCAATAAGGCACCACCCACCTATGATACTGTGCTACAGATGGAGTATCTTGACATGGTG
GTGAATGAAACGCTCAGATTATTCCCAATTGCTATGAGACTTGAGAGGGTCTGCAAAAAA
GATGTTGAGATCAATGGGATGTTCATTCCCAAAGGGTGGGTGGTGATGATTCCAAGCTAT
GCTCTTCACCGTGACCCAAAGTACTGGACAGAGCCTGAGAAGTTCCTCCCTGAAAGATTC
AGCAAGAAGAACAAGGACAACATAGATCCTTACATATACACACCCTTTGGAAGTGGACCC
AGAAACTGCATTGGCATGAGGTTTGCTCTCATGAACATGAAACTTGCTCTAATCAGAGTC
CTTCAGAACTTCTCCTTCAAACCTTGTAAAGAAACACAGATCCCCCTGAAATTAAGCTTA
GGAGGACTTCTTCAACCAGAAAAACCCGTTGTTCTAAAGGTTGAGTCAAGGGATGGCACC
GTAAGTGGAGCCTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID CYP3A3 Link Image
Target 2 GenAtlas ID CYP3A3 Link Image
Target 2 HGNC ID HGNC:2636 Link Image
Target 2 Chromosome Location 7
Target 2 Locus 7q21.1
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Molowa DT, Schuetz EG, Wrighton SA, Watkins PB, Kremers P, Mendez-Picon G, Parker GA, Guzelian PS: Complete cDNA sequence of a cytochrome P-450 inducible by glucocorticoids in human liver. Proc Natl Acad Sci U S A. 1986 Jul;83(14):5311-5. [PubMed Link Image]
  2. Watkins PB, Wrighton SA, Maurel P, Schuetz EG, Mendez-Picon G, Parker GA, Guzelian PS: Identification of an inducible form of cytochrome P-450 in human liver. Proc Natl Acad Sci U S A. 1985 Sep;82(18):6310-4. [PubMed Link Image]
Target 2 Drug References
  1. Saw J, Steinhubl SR, Berger PB, Kereiakes DJ, Serebruany VL, Brennan D, Topol EJ: Lack of adverse clopidogrel-atorvastatin clinical interaction from secondary analysis of a randomized, placebo-controlled clopidogrel trial. Circulation. 2003 Aug 26;108(8):921-4. Epub 2003 Aug 18. [PubMed Link Image]
  2. Neubauer H, Gunesdogan B, Hanefeld C, Spiecker M, Mugge A: Lipophilic statins interfere with the inhibitory effects of clopidogrel on platelet function--a flow cytometry study. Eur Heart J. 2003 Oct;24(19):1744-9. [PubMed Link Image]
  3. Lau WC, Gurbel PA, Watkins PB, Neer CJ, Hopp AS, Carville DG, Guyer KE, Tait AR, Bates ER: Contribution of hepatic cytochrome P450 3A4 metabolic activity to the phenomenon of clopidogrel resistance. Circulation. 2004 Jan 20;109(2):166-71. Epub 2004 Jan 5. [PubMed Link Image]
  4. Mukherjee D, Kline-Rogers E, Fang J, Munir K, Eagle KA: Lack of clopidogrel-CYP3A4 statin interaction in patients with acute coronary syndrome. Heart. 2005 Jan;91(1):23-6. [PubMed Link Image]
  5. Poulsen TS, Vinholt P, Mickley H, Korsholm L, Kristensen SR, Damkier P: Existence of a clinically relevant interaction between clopidogrel and HMG-CoA reductase inhibitors? Re-evaluating the evidence. Basic Clin Pharmacol Toxicol. 2005 Feb;96(2):103-10. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 2058
Target 3 Name P-selectin
Target 3 Synonyms
  1. CD62P antigen
  2. GMP-140
  3. Granule membrane protein 140
  4. LECAM3
  5. Leukocyte-endothelial cell adhesion molecule 3
  6. P-selectin precursor
  7. PADGEM
Target 3 Gene Name SELP
Target 3 Protein Sequence >P-selectin precursor 
MANCQIAILYQRFQRVVFGISQLLCFSALISELTNQKEVAAWTYHYSTKAYSWNISRKYC
QNRYTDLVAIQNKNEIDYLNKVLPYYSSYYWIGIRKNNKTWTWVGTKKALTNEAENWADN
EPNNKRNNEDCVEIYIKSPSAPGKWNDEHCLKKKHALCYTASCQDMSCSKQGECLETIGN
YTCSCYPGFYGPECEYVRECGELELPQHVLMNCSHPLGNFSFNSQCSFHCTDGYQVNGPS
KLECLASGIWTNKPPQCLAAQCPPLKIPERGNMICLHSAKAFQHQSSCSFSCEEGFALVG
PEVVQCTASGVWTAPAPVCKAVQCQHLEAPSEGTMDCVHPLTAFAYGSSCKFECQPGYRV
RGLDMLRCIDSGHWSAPLPTCEAISCEPLESPVHGSMDCSPSLRAFQYDTNCSFRCAEGF
MLRGADIVRCDNLGQWTAPAPVCQALQCQDLPVPNEARVNCSHPFGAFRYQSVCSFTCNE
GLLLVGASVLQCLATGNWNSVPPECQAIPCTPLLSPQNGTMTCVQPLGSSSYKSTCQFIC
DEGYSLSGPERLDCTRSGRWTDSPPMCEAIKCPELFAPEQGSLDCSDTRGEFNVGSTCHF
SCNNGFKLEGPNNVECTTSGRWSATPPTCKGIASLPTPGLQCPALTTPGQGTMYCRHHPG
TFGFNTTCYFGCNAGFTLIGDSTLSCRPSGQWTAVTPACRAVKCSELHVNKPIAMNCSNL
WGNFSYGSICSFHCLEGQLLNGSAQTACQENGHWSTTVPTCQAGPLTIQEALTYFGGAVA
STIGLIMGGTLLALLRKRFRQKDDGKCPLNPHSHLGTYGVFTNAAFDPSP
Target 3 Number of Residues 843
Target 3 Molecular Weight 90845
Target 3 Theoretical pI 6.64
Target 3 GO Classification
Function
binding
carbohydrate binding
sugar binding
Process
cellular process
cell adhesion
Component
cell
membrane
Target 3 General Function Involved in sugar binding
Target 3 Specific Function Ca(2+)-dependent receptor for myeloid cells that binds to carbohydrates on neutrophils and monocytes. Mediates the interaction of activated endothelial cells or platelets with leukocytes. The ligand recognized is sialyl-Lewis X
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • 1-41
Target 3 Transmembrane Regions
  • 772-795
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 183389 Link Image
Target 3 UniProtKB/Swiss-Prot ID P16109 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name LYAM3_HUMAN Link Image
Target 3 PDB ID 1G1S Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Membrane
  • single-pass type I membrane protein
Target 3 Gene Sequence >2493 bp 
ATGGCCAACTGCCAAATAGCCATCTTGTACCAGAGATTCCAGAGAGTGGTCTTTGGAATT
TCCCAACTCCTTTGCTTCAGTGCCCTGATCTCTGAACTAACAAACCAGAAAGAAGTGGCA
GCATGGACTTATCATTACAGCACAAAAGCATACTCATGGAATATTTCCCGTAAATACTGC
CAGAATCGCTACACAGACTTAGTGGCCATCCAGAATAAAAATGAAATTGATTACCTCAAT
AAGGTCCTACCCTACTACAGCTCCTACTACTGGATTGGGATCCGAAAGAACAATAAGACA
TGGACATGGGTGGGAACCAAAAAGGCTCTCACCAACGAGGCTGAGAACTGGGCTGATAAT
GAACCTAACAACAAAAGGAACAACGAGGACTGCGTGGAGATATACATCAAGAGTCCGTCA
GCCCCTGGCAAGTGGAATGATGAGCACTGCTTGAAGAAAAAGCACGCATTGTGTTACACA
GCCTCCTGCCAGGACATGTCCTGCAGCAAACAAGGAGAGTGCCTCGAGACCATCGGGAAC
TACACCTGCTCCTGTTACCCTGGATTCTATGGGCCAGAATGTGAATACGTGAGAGAGTGT
GGAGAACTTGAGCTCCCTCAACACGTGCTCATGAACTGCAGCCACCCTCTGGGAAACTTC
TCTTTTAACTCGCAGTGCAGCTTCCACTGCACTGACGGGTACCAAGTAAATGGGCCCAGC
AAGCTGGAATGCTTGGCTTCTGGAATCTGGACAAATAAGCCTCCACAGTGTTTAGCTGCC
CAGTGCCCACCCCTGAAGATTCCTGAACGAGGAAACATGATCTGCCTTCATTCTGCAAAA
GCATTCCAGCATCAGTCTAGCTGCAGCTTCAGTTGTGAAGAGGGATTTGCATTAGTTGGA
CCGGAAGTGGTGCAATGCACAGCCTCGGGGGTATGGACAGCCCCAGCCCCAGTGTGTAAA
GCTGTGCAGTGTCAGCACCTGGAAGCCCCCAGTGAAGGAACCATGGACTGTGTTCATCCG
CTCACTGCTTTTGCCTATGGCTCCAGCTGCAAATTTGAGTGCCAGCCCGGCTACAGAGTG
AGGGGCTTGGACATGCTCCGCTGCATTGACTCTGGACACTGGTCTGCACCCTTGCCAACC
TGTGAGGCTATTTCGTGTGAGCCGCTGGAGAGTCCTGTCCACGGAAGCATGGATTGCTCT
CCATCCTTGAGAGCGTTTCAGTATGACACCAACTGTAGCTTCCGCTGTGCTGAAGGTTTC
ATGCTGAGAGGAGCCGATATAGTTCGGTGTGATAACTTGGGACAGTGGACAGCACCAGCC
CCAGTCTGTCAAGCTTTGCAGTGCCAGGATCTCCCAGTTCCAAATGAGGCCCGGGTGAAC
TGCTCCCACCCCTTCGGTGCCTTTAGGTACCAGTCAGTCTGCAGCTTCACCTGCAATGAA
GGCTTGCTCCTGGTGGGAGCAAGTGTGCTACAGTGCTTGGCTACTGGAAACTGGAATTCT
GTTCCTCCAGAATGCCAAGCCATTCCCTGCACACCTTTGCTAAGCCCTCAGAATGGAACA
ATGACCTGTGTTCAACCTCTTGGAAGTTCCAGTTATAAATCCACATGTCAATTCATCTGT
GACGAGGGATATTCTTTGTCTGGACCAGAAAGATTGGATTGTACTCGATCGGGACGCTGG
ACAGACTCCCCACCAATGTGTGAAGCCATCAAGTGCCCAGAACTCTTTGCCCCAGAGCAG
GGCAGCCTGGATTGTTCTGACACTCGTGGAGAATTCAATGTTGGCTCCACCTGTCATTTC
TCTTGTAACAATGGCTTTAAGCTGGAGGGGCCCAATAATGTGGAATGCACAACTTCTGGA
AGATGGTCAGCTACTCCACCAACCTGCAAAGGCATAGCATCACTTCCTACTCCAGGGTTG
CAATGTCCAGCCCTCACCACTCCTGGGCAGGGAACCATGTACTGTAGGCATCATCCGGGA
ACCTTTGGTTTTAATACCACTTGTTACTTTGGCTGCAACGCTGGATTCACACTCATAGGA
GACAGCACTCTCAGCTGCAGACCTTCAGGACAATGGACAGCAGTAACTCCAGCATGCAGA
GCTGTGAAATGCTCAGAACTACATGTTAATAAGCCAATAGCGATGAACTGCTCCAACCTC
TGGGGAAACTTCAGTTATGGATCAATCTGCTCTTTCCATTGTCTAGAGGGCCAGTTACTT
AATGGCTCTGCACAAACAGCATGCCAAGAGAATGGCCACTGGTCAACTACCGTGCCAACC
TGCCAAGCAGGACCATTGACTATCCAGGAAGCCCTGACTTACTTTGGTGGAGCGGTGGCT
TCTACAATAGGTCTGATAATGGGTGGGACGCTCCTGGCTTTGCTAAGAAAGCGTTTCAGA
CAAAAAGATGATGGGAAATGCCCCTTGAATCCTCACAGCCACCTAGGAACATATGGAGTT
TTTACAAACGCTGCATTTGACCCGAGTCCTTAA
Target 3 GenBank Gene ID
Target 3 GeneCard ID SELP Link Image
Target 3 GenAtlas ID SELP Link Image
Target 3 HGNC ID HGNC:10721 Link Image
Target 3 Chromosome Location 1
Target 3 Locus 1q22-q25
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed Link Image]
  2. Florian V, Schluter T, Bohnensack R: A new member of the sorting nexin family interacts with the C-terminus of P-selectin. Biochem Biophys Res Commun. 2001 Mar 9;281(4):1045-50. [PubMed Link Image]
  3. Johnston GI, Cook RG, McEver RP: Cloning of GMP-140, a granule membrane protein of platelets and endothelium: sequence similarity to proteins involved in cell adhesion and inflammation. Cell. 1989 Mar 24;56(6):1033-44. [PubMed Link Image]
  4. Bajorath J, Stenkamp R, Aruffo A: Knowledge-based model building of proteins: concepts and examples. Protein Sci. 1993 Nov;2(11):1798-810. [PubMed Link Image]
  5. Fujimoto T, Stroud E, Whatley RE, Prescott SM, Muszbek L, Laposata M, McEver RP: P-selectin is acylated with palmitic acid and stearic acid at cysteine 766 through a thioester linkage. J Biol Chem. 1993 May 25;268(15):11394-400. [PubMed Link Image]
  6. Freedman SJ, Sanford DG, Bachovchin WW, Furie BC, Baleja JD, Furie B: Structure and function of the epidermal growth factor domain of P-selectin. Biochemistry. 1996 Oct 29;35(43):13733-44. [PubMed Link Image]
  7. Herrmann SM, Ricard S, Nicaud V, Mallet C, Evans A, Ruidavets JB, Arveiler D, Luc G, Cambien F: The P-selectin gene is highly polymorphic: reduced frequency of the Pro715 allele carriers in patients with myocardial infarction. Hum Mol Genet. 1998 Aug;7(8):1277-84. [PubMed Link Image]
Target 3 Drug References
  1. Neubauer H, Gunesdogan B, Hanefeld C, Spiecker M, Mugge A: Lipophilic statins interfere with the inhibitory effects of clopidogrel on platelet function--a flow cytometry study. Eur Heart J. 2003 Oct;24(19):1744-9. [PubMed Link Image]
  2. Massberg S, Mueller I, Besta F, Thomas P, Gawaz M: Effects of 2 different antiplatelet regimens with abciximab or tirofiban on platelet function in patients undergoing coronary stenting. Am Heart J. 2003 Nov;146(5):E19. [PubMed Link Image]
  3. Dalby M, Montalescot G, Bal dit Sollier C, Vicaut E, Soulat T, Collet JP, Choussat R, Gallois V, Drobinski G, Drouet L, Thomas D: Eptifibatide provides additional platelet inhibition in non-ST-elevation myocardial infarction patients already treated with aspirin and clopidogrel. Results of the platelet activity extinction in non-Q-wave myocardial infarction with aspirin, clopidogrel, and eptifibatide (PEACE) study. J Am Coll Cardiol. 2004 Jan 21;43(2):162-8. [PubMed Link Image]
  4. Angiolillo DJ, Fernandez-Ortiz A, Bernardo E, Ramirez C, Sabate M, Hernandez-Antolin R, Moreno R, Escaned J, Alfonso F, Banuelos C, Macaya C: Is a 300 mg clopidogrel loading dose sufficient to inhibit platelet function early after coronary stenting? A platelet function profile study. J Invasive Cardiol. 2004 Jun;16(6):325-9. [PubMed Link Image]
  5. Kastrati A, von Beckerath N, Joost A, Pogatsa-Murray G, Gorchakova O, Schomig A: Loading with 600 mg clopidogrel in patients with coronary artery disease with and without chronic clopidogrel therapy. Circulation. 2004 Oct 5;110(14):1916-9. Epub 2004 Jul 19. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.